1. Field of Invention
Antitumor compositions comprising avarol and method of employing avarol for its antitumor activity; method of and ameliorating, alleviating, or palliating tumorous and/or cancerous conditions therewith; method of production of the active principles avarol. In brief, pharmaceutical compositions embodying avarol, method of treating with avarol, and employment of the said active principles for its anticarcinogenic activity as.
It is to be understood that, any suggestion in this application to the contrary notwithstanding, the present invention is directed only to a method of combating tumor cells, the growth of which is adversely affected by Avarol and therefore susceptible thereto, comprising the step of administering to the host an effective antitumor amount of Avarol, advantageously in the form of a pharmaceutical composition thereof in which it is present together with a pharmaceutically-acceptable carrier or diluent, and to antitumor pharmaceutical compositions which are effective and therefore useful for such purpose.
2. Prior Art
Avarone and its hydroquinone derivative avarol are natural substances found in the marine sponge Dysidea avara (L. Minale, R. Riccio and G. Sodano, Tetrahedron Letters 1974, 3401-3404; S. de Rosa, L. Minale, R. Riccio and G. Sodano, J. Chem. Soc. Perkin I, 1408-1414 (1976)). These compounds were isolated from a diethyl ether extract using column chromatography on silica gel (L. Cariello, M. de Nicola Giudici and L. Zanetti, Comp. Biochem. Physiol. 65c, 37-41 (1980)). With regard to biological effects it has so far only been known that avarol in very high concentrations (130 .mu.m) affects the cells of the sea urchin embryo, causing "developmental abberations" (L. Cariello et al., ibid.). The derivatives described in the literature are, among others, the 3'-methylamino and the 4'-methylaminoavarone (G. Cimino, S. de Rosa, S. de Stefano, L. Cariello and L. Zanetti, Experientia 38, 896 (1982) as well as the avarol dimethyl ether and the avarol diacetate (S. de Rosa et al., ibid.).